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01/31/08 - USPTO Class 424 |  87 views | #20080026086 | Prev - Next | About this Page  424 rss/xml feed  monitor keywords

Synergistic neuroprotective, combinations of flavanols, hydroxystilbenes, flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins

USPTO Application #: 20080026086
Title: Synergistic neuroprotective, combinations of flavanols, hydroxystilbenes, flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins
Abstract: A synthetic composition is provided comprising (a) one or more compounds selected from the group consisting of flavanols and hydroxystilbenes; and (b) one or more compounds selected from the group consisting of flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins. Also provided is a method of reducing neuronal degeneration in an individual which method comprises administering to the individual said composition. (end of abstract)



Agent: Unilever Intellectual Property Group - Englewood Cliffs, NJ, US
Inventors: Caroline Dawn Holyoak, Karen Thethi
USPTO Applicaton #: 20080026086 - Class: 424770 (USPTO)

Synergistic neuroprotective, combinations of flavanols, hydroxystilbenes, flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins description/claims


The Patent Description & Claims data below is from USPTO Patent Application 20080026086, Synergistic neuroprotective, combinations of flavanols, hydroxystilbenes, flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins.

Brief Patent Description - Full Patent Description - Patent Application Claims
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FIELD OF THE INVENTION

[0001]The present invention relates to composition comprising combinations of polyphenols and their use in reducing neuronal degeneration in the hippocampus.

BACKGROUND TO THE INVENTION

[0002]Public awareness and concerns about a number of disease states which exhibit age related decline in cognitive function have increased in recent years. These conditions are known by a number of names including dementia, senility, age-related amnesia and Alzheimer's syndrome. Although research is ongoing worldwide for pharmaceutical agents which delay or halt the decline in cognitive function, there remains a risk that the associated physiological changes are partially or totally irreversible. Therefore, there would be a clear benefit if an agent or agents could be found, preferably derivable from natural products, which could be administered by way of the normal human diet or supplementary thereto, which could have at least some prophylactic or therapeutic activity in respect of these conditions. Such agents could, for example, be used from an early age before cognitive decline presents clinically.

SUMMARY OF THE INVENTION

[0003]We have now found that particular combinations of classes of polyphenols exhibit synergistic activity in assays indicative of an ability to delay, reduce or prevent age related decline in cognitive function.

[0004]Accordingly, in a first aspect, the present invention provides A synthetic composition comprising (a) one or more compounds selected from the group consisting of flavanols and hydroxystilbenes; and (b) one or more compounds selected from the group consisting of flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins with the proviso that a combination of (i) catechin and quercetin and (ii) EGCg, pine extract and grape extract is specifically excluded; [0005]wherein the molar ratio of total group (a) compound(s) to total group (b) compound(s) in said composition is at least 2.5:1.

[0006]As used herein, the term "synthetic composition" means a composition which is not per se found in nature and is at least in part modified from a natural source and/or at least partially produced by synthetic organic chemistry.

[0007]Preferably (a) comprises one or more flavanols and (b) comprises one or more flavonols.

[0008]The present invention also provides a medicament or nutritional supplement comprising a composition of the invention together with a pharmacologically acceptable carrier. The present invention further provides a food product comprising a composition of the invention and a beverage comprising a composition of the invention.

[0009]In a second aspect, the present invention provides a method of reducing neuronal degeneration in an individual which method comprises administering to the individual, an effective amount of a composition which comprises (a) one or more compounds selected from the group consisting of flavanols and hydroxystilbenes; and (b) one or more compounds selected from the group consisting of flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins. Also provided is the use of said composition in the manufacture of a medicament for use in reducing neuronal degeneration in an individual.

[0010]In a third aspect, the present invention provides a method of delaying, reducing or preventing an age-related decline in cognitive function in a mammal such as human which method comprises administering to the mammal an effective amount of a composition which comprises (a) one or more compounds selected from the group consisting of flavanols and hydroxystilbenes; and (b) one or more compounds selected from the group consisting of flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins. Also provided is the use of said composition in the manufacture of products capable of delaying, reducing or preventing an age related decline in cognitive function in a mammal such as a human.

DETAILED DESCRIPTION OF THE INVENTION

[0011]Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art.

[0012]Compositions according to the present invention comprise one or more compounds of group (a) as hereinbefore defined and one or more compounds of group (b) as hereinbefore defined. Preferably, the total molar ratio of group (a) compound(s) to group (b) compound(s) is at least 2.5:1, more preferably at least 3:1, more preferably at least 4:1. Preferably, the total molar ratio of group (a) compound(s) to group (b) compound(s) is less than 50:1.

[0013]Compounds of group (a) are selected from flavanols and hydroxystilbenes. Flavanols include catechin, epicatechin, gallocatechin, epigallocatechin, and esters thereof with gallic acid, i.e. catechin gallate epicatechin gallate, gallocatechin gallate and epigallocatechin gallate (EGCg). Preferred flavanols have one or more gallate moieties. Hydroxystilbenes include resveratrol and oxyresveratrol.

[0014]The compounds can be chemically synthesised or obtained from plant materials. For example, epigallocatechin gallate can be obtained from green tea extract.

[0015]Compounds of group (b) are selected from flavanones, flavones, flavonols, proanthocyanidins and anthocyanidins.

[0016]Flavanones include naringenin, hesperitin sakranetin. Flavones include luteolin and apigenin. Flavonols include quercitin, kaempferol and myricetin. Flavonols exist in nature as the aglycone or as O-glycosides. Glycosylated forms are preferred.

[0017]Again, the compounds can be chemically synthesised or obtained from plant materials. For example, in a preferred embodiment, a mixture of proanthocyanidins and anthocyanidins is provided as an extract of the bark of French maritime pine (Pinus pinatus). One such extract is available commercially as Pycnogenol.TM..

[0018]A plant extract differs from the intact plant material in that the various components present in the intact plant material will be present in different amounts in the extract, or substantially absent. Prior to extraction, plant materials may be dried and or mechanically processed, e.g. crushed.

[0019]Extracts of plant materials are typically made by solvent extraction. Solvents include "solvent" includes polar and non-polar organic solvents, water, and mixtures thereof. Preferred solvents are water, ethanol and mixtures thereof. Extraction procedures may include a heating step. Solvent extracted components may be subject to further purification/separation steps such as chromatography or fractional distillation. As used herein, "fraction" means any fractioned part of a solvent containing one or more of the active ingredients described above, e.g. obtained by chromatography or by fractional distillation.

[0020]Suitable plant sources of the various polyphenolic compounds described above include tea, fresh fruit such as grapes (skin and seeds in particular), cranberry, blackcurrants, blackberries and citrus fruits, and vegetables such as onions, kale, broccoli and French beans.

[0021]The solubility of flavonols in aqueous solvents can be increased by co-dissolving one or more anthocyanidins (see U.S. Pat. No. 6,569,446).

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Brief Patent Description - Full Patent Description - Patent Application Claims

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